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Pharmacological properties

otilonium bromide is a typical representative of the class of drugs based on the quaternary salt of 2-aminoethyl-n-benzylaminobenzoate.

Otilonium bromide has an antispasmodic effect on the smooth muscles of the distal intestine (colon and rectum). This effect is noted when using doses that do not affect gastric secretion and do not cause typical atropine-like side effects.

Mechanism of action. Otilonium bromide acts primarily by changing the current of Ca ions2+ between the intracellular and extracellular space, reducing the trigger factor of contractile activity. Otilonium bromide inhibits the opening of L-type calcium channels and the penetration of Ca ions2+ into the smooth muscles of the intestines. An additional pharmacodynamic effect is achieved by inhibiting tachykinin and muscarinic receptors.

Clinical efficacy and safety. An extended analysis of a double-blind, placebo-controlled 15-week study of otilonium bromide (SpC1M study) conducted in 378 patients with irritable bowel syndrome (IBS) showed that the frequency of therapeutic response for 2–4 months was significantly higher in the otilonium bromide group (36.9%) compared with the placebo group (22.5%; p = 0.007). Each month, the frequency of achievement of the therapeutic response was higher in the otilonium bromide group compared with placebo (p0.05). The total monthly and weekly part of the population with a therapeutic response for individual endpoints (intensity and frequency of pain and discomfort, flatulence / bloating, severity of diarrhea and constipation, mucus in the feces) was significantly higher in the otilonium bromide group compared with the placebo group range of differences from 10 to 20%. Analysis of the results of bowel movements and stool consistency indicates that additional benefits are seen in patients with diarrhea. Safety data for the use of otilonium bromide is similar to placebo.

A double-blind, placebo-controlled clinical study (n = 365 patients with IBS) (OBIS study) confirmed the effectiveness of otilonium bromide compared with placebo in reducing the frequency of abdominal pain, the degree of bloating and the prevention of recurrence of symptoms.

Pharmacokinetics It is believed that otilonium bromide penetrates the site of pharmacological action through the intestinal wall, since the systemic absorption of the drug after oral administration is very low (3%). Therefore, its concentration in blood plasma is low. After oral administration, a high distribution of the drug in the smooth muscles of the colon and rectum is described. The use of the drug shortly before meals provides a pharmacologically effective local bioavailability of the drug at the site of therapeutic action and while waiting for the most pronounced symptoms of the disease. The use of otilonium bromide in patients with impaired renal and hepatic function has not been investigated. Since otilonium bromide enters the systemic circulation in extremely small quantities, impaired renal and hepatic function is not expected.

Preclinical Safety Data

Acute toxicity: with oral administration in dogs of doses up to 1000 mg / kg, no deaths were reported, and with oral administration in rats DL50 was 1500 mg / kg.

Chronic toxicity: when using otilonium bromide at a dose of 80 mg / kg for 180 days, the animals did not show any hematological or histological disorders.

Embryotoxicity: no embryotoxic and teratogenic effects were observed with doses up to 60 mg / kg in rats and rabbits.

Genotoxicity: standard in vitro and in vivo clinical trials did not reveal any mutagenic potential for otilonium bromide.

Indications

Symptomatic treatment of cystic arthritis and spastic pain in the distal intestines (colon and rectum), reduction of abdominal pain, bloating and peristalsis caused by smooth muscle spasm of the distal intestines in patients aged ≥18 years.

Treatment of IBS should begin with non-pharmacological measures (lifestyle changes, diet, emotional support, psychotherapy), pharmacotherapy is prescribed when such measures do not have the desired effect.

Application

Mode of application. tablets should be swallowed whole with a glass of water. tablets should be taken 20 minutes before meals.

Doses The recommended single dose is 1 tablet of 40 mg, the recommended daily dose is 80-120 mg (1 tablet 2-3 times a day). The dose depends on the clinical picture and response to treatment, the drug should be prescribed in accordance with the therapeutic guidelines for the treatment of IBS.

The duration of treatment depends on the course of the disease. Doctors should periodically evaluate the need for continued therapy.

Special patient groups

Patients with impaired liver and kidney function. No dose changes are required (see Pharmacokinetics for details).

Elderly patients. A change in the dose of the drug is not required.

Children. Clinical data on the use of the drug in patients under the age of 18 years are limited, therefore it is not intended for use in children.

Contraindications

The presence in the history of a hypersensitivity reaction to the active substance or any component of the drug.

Side effects

In clinical studies, the drug spasmomen well tolerated; an insignificant number of adverse reactions were reported that were similar in nature to the reactions with the use of a placebo / reference drug (see table).

The frequency of adverse reactions in patients taking otilonium bromide can be classified as follows: often (from ≥1 / 100 to 1/10), infrequently (from ≥1 / 1000 to 1/100), rarely (from ≥1 / 10,000 to 1/1000).

Table. Adverse reactions reported during clinical trials

From the gastrointestinal tract Uncommon: dry mouth, nausea, pain in the upper abdomen
On the part of the skin and subcutaneous tissue Infrequently: itching, erythema
General disorders and disorders at the injection site Infrequently: weakness, asthenia
From the nervous system Infrequently: headache
On the part of the organ of hearing and the labyrinth Infrequently: dizziness

In post-marketing studies, individual cases of hypersensitivity reactions from the skin (urticaria, angioedema) were reported. Such cases were reported voluntarily in an indefinite population, which makes it impossible to reliably estimate their frequency, therefore it is unknown.

Reported suspected adverse reactions. Reporting suspected adverse reactions after drug registration plays an important role. This allows you to continue monitoring the benefit / risk ratio of this drug.

Health care workers should report any suspected adverse reactions through the national alert system.

special instructions

The drug should be used with caution in glaucoma, prostatic hypertrophy and pyloric stenosis.

The drug contains lactose, therefore it is contraindicated in patients with lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome.

Use during pregnancy and lactation. There are no clinical data on the use of the drug Spasmomen during pregnancy and lactation. During animal studies, Spasmomen did not exhibit embryotoxic, teratogenic or mutagenic effects, nor did he exhibit reproductive and ontogenetic toxicity.However, like all medicines, it can be used during pregnancy and lactation only if absolutely necessary and under close medical supervision.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. The spasmomen does not affect or has an extremely insignificant effect on the reaction rate when driving vehicles or other mechanisms.

Interactions

Studies of the interaction of otilonium bromide with other drugs have not been conducted. It is assumed that taking otilonium bromide in the recommended daily dose of 1 tablet 2 or 3 times a day during the passage of the gastrointestinal tract will not affect the absorption of other oral drugs used simultaneously.

Overdose

In animal studies, otilonium bromide had practically no toxic effect when using doses many times higher than the usual pharmacological dose (for detailed information, see preclinical safety data). therefore, it is assumed that with an overdose of a drug in a person, no serious violations should occur. in case of overdose, symptomatic supportive therapy is recommended.

Storage conditions

Special storage conditions are not required.

Tags: Otilonium bromide